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Pharmacology Test 2 > Estrogens, Progestins, & Their Antagonist > Flashcards

Estrogens, Progestins, & Their Antagonist Flashcards

(60 cards)

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1
Q

Estrogens

A
  • critical for sexual development and 2nd characteristics

- stimulate growth of uterine muscle & endometrial lining

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2
Q

3 human nature estrogens

A

E1: estrone
E2: estradiol
E3: estriol

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3
Q

Strongest most potent estrogen

A

E2 (80x) > E1 (8x) > E3 (1x)

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4
Q

Metabolic & Cardiovascular Effects of Estrogen

Blood, Lipid, Bone

A

(good) Bone: increase formation, decrease resorption, increase height, decrease muscle mass
(good) Lipid: increase HDL, VLDL, TG; decrease LDL, total cholesterol, fat deposition; increase fat metabolism
(bad) Blood: increase coagulation factors, increase coagulability of blood, increase risk of blood clots

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5
Q

Estrogen Receptors

ERa ERb

A

made from two different genes
ERa: endometrium
ERb: kidney, brain

E2 binds both receptors; E1 prefers ERa; E3 prefers ERb

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6
Q

Estrogen is expressed mainly in

A

bone, heart, breast

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7
Q

ERa

A

endometrium; over expressed in breast cancer

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8
Q

Estrogen Mechanism of Action

A
  • estrogen cross cell membrane and bind ERa/b
  • conformational change
  • interacts with coregulators
  • coregulators may affect tissue-specific effects of selective estrogen receptor modulators (SERM)
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9
Q

ERb vs ERa

A

ERb has its own separate action, and may have a dominant negative effect on ERa

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10
Q

ERa/b are made from

A

two different genes

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11
Q

Biosynthesis of Estrogens

Premenopausal

A

producing mainly E2 upon FSH stimulation

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12
Q

Biosynthesis of Estrogens

Postmenopausal

A

producing mainly E1

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13
Q

Biosynthesis of Estrogens

Pregnancy

A

producing mainly E3

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14
Q

Biosynthesis of Estrogens

Men

A

producing small amounts of E1 & E2

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15
Q

Main target for drug therapy

A

Aromatase

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16
Q

Ethinyl Estradiol EE

A

Synthetic Estrogen

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17
Q

Diethylstilbestrol DES

A

no longer used; hurt babies

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18
Q

Commonly used Estrogens

A 
Ethinyl Estradiol
Micronized estradiol
Estradiol cypionate
Estradiol valerate
Estropipate

ESTRADIOL & ESTROPIPATE

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19
Q

17a-ethinylestradiol

A

as active as E2

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20
Q

Mestranol

A
  • converted into 17aEE by liver

- chemical alterations increase oral bioavailability

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21
Q

Estrogen modifications

A

delay metabolism, increasing oral bioavailability

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22
Q

Clinical Uses of Estrogens

Primary Hypogonadism

A
  • replacement therapy in estrogen-deficient patients
  • attempts to mimic the physiology of puberty
  • chronic maintenance therapy consists of both estrogens and progestins
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23
Q

Clinical Uses of Estrogens
HRT
Postmenopausal Hormone Therapy

A
  • use estrogen/progestin to make up for declines after menopause

relieving symptoms including:

  • hot flashes
  • drying itchiness
  • sleep disturbances

USE SHOREST AND LOWEST POSSIBLE because potential risks

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24
Q

Estrogens for HRT

A

E1, E2, E3

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25
Estrogens for HRT | E1
- estropipate | - CCE, PREMARIN (conjugated equine estrogens)
26
Estrogens for HRT | E2
- attached to acetate, valerate, and cypionate groups that are hydrolyzed away in the body to produce estradiol
27
Estrogens for HRT | E3
- weak natural estrogen elevated during pregnancy | - ISNT converted into estrone; DOESNT INCREASE RISK OF BREAST OR ENDOMETRIAL CANCERS; higher dosage needed
28
ERa cancer
over expressed in breast cancer
29
Estrogen + Progestin for HRT
NEVER USE PROGESTIN ALONE; can use estrogen alone - CEE + MPA (medroxyprogesteron acetate) - indicated in women with a uterus - progesterone added to prevent endometrial hyperplasia from estrogen - added risks
30
Progestins
- need lots during pregnancy
31
Progesterone
- natural progestin in human - controls menstrual cycle, pregnancy - C21 steroid; precursor to other steroids
32
Name the Active Progesterone
P4
33
Biosynthesis of Progesterone | Non-pregnant women
- by granulosa lutein cells in corpus luteum | - LH stimulation
34
Biosynthesis of Progesterone | Pregnant women
- from corpus luteum | - hCG stimulation
35
Biosynthesis of Progesterone | 2nd month of pregnancy
- placenta secretes estriol and progesterone under delivery | - peaks third trimester
36
Progesterone Receptor A&B made by
ONE gene; different due to splicing
37
Need estrogen and progestin or
nada will happen (pregnancy wise)
38
MPA | Medroxyprogesterone Acetate
mixed with CEE estrogen for HRT
39
6 Progestational Agents
- progesterone - hydroxyprogesterone - medroxyprogesterone - dimethisterone - norethindrone - desogestrel
40
Most Important use of Progestins
Hormonal Contraception | - can use just progestin but usually with estrogen
41
Therapeutic Applications of Progestins
- HRT (w/ estrogen, never alone) - Long-term ovarian suppression - diagnostic uses: test estrogen secretion - hormonal contraception
42
Norgestrel | aka Norethindrone
Progestin-ONLY Pills - taken daily ectopic pregnancy risk - less effective than combination pills
43
Levonorgestrel
Plan B - ONLY progestin - use within 3 days; sooner = better
44
Ulipristal Acetate
SPRM Selective PR modulator Emergency Contraceptive
45
Mechanism of Hormonal Contraceptives
1) suppress ovulation 2) affects viscosity of mucus fluid and mobility and secretion of the uterine tubes (sperm can't reach egg) 3) interfere with implantation
46
Tamoxifen
Selective Estrogen Receptor Modulator (SERM) - nonsteroidal, antagoinst on the breast, and partial agonist on uterine and bone - palliative care for ER+ breast cancer - decreases total cholesterol - -- does not increase HDL and triglyceride
47
Rolaxifene
Selective Estrogen Receptor Modulator - nonsteroidal partial agonist on bone and antagonist on uterus and breast * ** same as tamoxifen EXCEPT less uterine cancer risk ***
48
Fulvestrant
Anti-estrogen - estrogen receptor - analog of estradiol with no known estrogenic activity - indicated for ER-positive metastatic breast cancer when resistant to Tamoxifen - degrades ERa receptor - affects fetus
49
Mifepristone
Anti-progestin - progestin receptor - PR and GR antagonist with luteolytic properties - medical abortion
50
Selective Estrogen Receptor Modulator | SERM
- tissue-selective estrogenic actions - Agonist: bone & CVS - Antagoinst: Breast & uterus
51
Toremifene
similar to Tamoxifen
52
Aromatase Inhibitors | Type 1
- Irreversible | - Steroidal
53
Exemestane
Aromatase Type I Inhibitor - binds irreversibly to aromatase - for postmenopausal women with ER+ early breast cancer - MORE EFFECTIVE than tamoxifen
54
Aromatase | Type 2
- reversible | - nonsteroidal
55
Anastrozole
Aromatase Type II Inhibitor - for ER+ breast cancer; first line treatment or following tamoxifen - sometimes helps ER- - NO RISK OF UTERINE CANCER OR DVT
56
Letrozole
Aromatase Type II Inhibitor - ER+ breast cancer - block estrogen production, increase FSH, stimulate follicle growth
57
Formestane
Aromatase Type I Inhibitor - irreversible - steroidal - similar to exemestane - weak androgen, mild AI; poor oral availability; no longer popular
58
Bazedoxifene
SERM | - in combination with conjugated estrogens, approved as HRT and osteoporosis
59
Clomiphene
SERM - older partial agonist - ovulation-inducing agent
60
Progestins without androgenic activity include
- desogestrel - norgestimate - gestodene

Pharmacology Test 2 (8 decks)

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